Maximizing Gabapentin bioavailability.

[Prescottdave]

For some reason, dextromethorphan massively potentiates GBP. Even just a regular 15mg dose can boost 100mg to the 1800mg level. Trust me, it's not placebo, I knew nothing about that interaction and was taking 60mg of Delsym every twelve hours, popped a cap of 100mg GBP and was messed up for almost two days. If you took 15mg of instant release (basically anything except Delsym), I'd imagine you'd get quite a rush.

Very true especially normal doses per the instructions on the back of the bottle. Same goes for many other z type drugs along with reducing thier WD symptoms. Though I find it does not potentiate it to the extent of the above post. Not something to do more then a couple times each year.

 

[Jarrikan]

first off please you guys need to be careful with DXM, for some people it is highly addictive, a deadly addiction that is hard to combat. Don't even go down that road. you will lose yourself and parts of your brain..

NOW Gabapentin is a great drug... the high that people describe... in my opinion is linked to personal psychology and behavior... now someone like me, who has extremely high social anxiety daily/constantly... would probably notice the "high" associated with this drug because it can make you very social... even strangely social, it can get you moving and doing things..
it can make things SEEM more fun, and of course the little waves of euphoria that are sometimes produced later in the dose are great.. if you are down alot and full of anxiety, you would probably get this side effect of the "nuerontin high" but is it really a high? or a mass reduction in ones own personal issues with behavior and psychology? What do you guys think?
Note - I've been on gabapentin for a number of years. i find it very helpful for social anxiety and overall mood stabilization, and i stagger my doses 300mg every 30-45 mins.

 

[Weltmeister]

first off please you guys need to be careful with DXM, for some people it is highly addictive, a deadly addiction that is hard to combat. Don't even go down that road. you will lose yourself and parts of your brain..

You could say that about most (if not every) drug

 

[Runningfox]

^^^^^Agreed. And not only substances but also behaviours. Gambling sex overeating..... the list is endless.

 

[Prescottdave]

first off please you guys need to be careful with DXM, for some people it is highly addictive, a deadly addiction that is hard to combat. Don't even go down that road. you will lose yourself and parts of your brain..

NOW Gabapentin is a great drug... the high that people describe... in my opinion is linked to personal psychology and behavior... now someone like me, who has extremely high social anxiety daily/constantly... would probably notice the "high" associated with this drug because it can make you very social... even strangely social, it can get you moving and doing things..
it can make things SEEM more fun, and of course the little waves of euphoria that are sometimes produced later in the dose are great.. if you are down alot and full of anxiety, you would probably get this side effect of the "nuerontin high" but is it really a high? or a mass reduction in ones own personal issues with behavior and psychology? What do you guys think?
Note - I've been on gabapentin for a number of years. i find it very helpful for social anxiety and overall mood stabilization, and i stagger my doses 300mg every 30-45 mins.

I found gabapentin was far more addictive physically then DXM which does not cause any type of significant cessation syndrome.

 

[Runningfox]

I found gabapentin was far more addictive physically then DXM which does not cause any type of significant cessation syndrome.

Wait which one are you saying didn't exhibit a cessation syndrome for you? The DXM or the gabapentin? I ask because gabapentin most Definately carried withdrawals for me.... still does when I lower dose in my months-long taper.

 

[quaintrelle]

I?ve been on gabapentin for 7 months now- 600 mg 3x/day (broke my neck). My tolerance is skkkyyyy high. I?ve been wanting to use it recreationally as I?ve read it?s all the rage these days. So- i came across this thread, followed RedLeaders advice and I feel freaking great! Stagger, folks... stagger!

 

[Runningfox]

I?ve been on gabapentin for 7 months now- 600 mg 3x/day (broke my neck). My tolerance is skkkyyyy high. I?ve been wanting to use it recreationally as I?ve read it?s all the rage these days. So- i came across this thread, followed RedLeaders advice and I feel freaking great! Stagger, folks... stagger!

You have a broken neck n all they gave you was gabapentin?

 

[Tubbs]

That's pretty fucked up, when I broke my ribs they basically threw painkillers at me.

 

[Pomzazed]

Lol, some part of the world opioids arent throw around like candy like in the US.

I, too, once have broken legbone which needs orthopedic cast, and the only meds i got were 500mg Acetaminophen and 300mg Gabapentin (bid).

 

[Thou]

Been on it years, 1800mg a day for anxiety. Usually always staggered 150mg every half hour until reached desired effect on account of rapid receptor saturation turning bioavailbility to shit.

Doesn't work for shit anymore so I'm taking a break. Lyrica is better but they both exacerbate my focus and attention problems.

 

[JacksinPA]

I've been taking gabapentin for years to treat the depression side of bipolar. At 100-200 mg 2-3 times/day, it's like taking sugar pills - no noticeable effects beyond a quick lifting of the anxiety/depression. But when I tried 2,000 mg in one shot on a mostly empty stomach, I had quite the pleasant buzz that evening. Subsequent experiences confirmed very rapid onset of tolerance which is said to go away after 5-7 weeks away from it in large doses.

There's a discussion on the Gabapentin High thread about this drug's bioavailability & absorption limits. That got me thinking about this molecule. Basically it is an amino acid with a big, fatty cyclohexane ring in its middle. This type of molecule is called zwitterionic as it contains both an acidic & a basic functional groups. That got me thinking about simple water-soluble acidic & basic salt derivatives that might significantly alter the drug's effects. The acid form could be the hydrochloride salt & the basic form could be the sodium salt. Both of these are known materials. See graphic:

I won't provide any synthesis ideas, so be careful as you may find yourself sailing on uncharted seas! I have not done a lit search on these 2 very different molecules so these are only my ideas & not guidance.

GabaP was developed at Parke-Davis years ago & I'm pretty sure they would have evaluated these 2 salt forms but chose to go with the neutral (zwitterionic) form for some very good reasons.

 

[Keif' Richards]

^TOLERANCE. It is the primary downside to these drugs, which aside from this aspect are wonderful in so many ways. I've never used these drugs daily for that reason. Even after 3 days of use, the effect is diminished to near geometric proportions. I've posted this in another thread actually, but I feel that the future will entail Gabapentinoid drugs that do not have this same propensity for inducing withdrawal.

I'm not going to give any medical advice, only comment on my personal experience. These drugs are best used on a sporadic basis. Tolerance develops too quickly. By using the drug sporadically, you really can maintain many of the positive benefits. I recommend no longer that 3 days, but again, this is only what has worked in my experience.

 

[Runningfox]

^TOLERANCE. It is the primary downside to these drugs, which aside from this aspect are wonderful in so many ways. I've never used these drugs daily for that reason. Even after 3 days of use, the effect is diminished to near geometric proportions. I've posted this in another thread actually, but I feel that the future will entail Gabapentinoid drugs that do not have this same propensity for inducing withdrawal.

I'm not going to give any medical advice, only comment on my personal experience. These drugs are best used on a sporadic basis. Tolerance develops too quickly. By using the drug sporadically, you really can maintain many of the positive benefits. I recommend no longer that 3 days, but again, this is only what has worked in my experience.

I second this. (*and your post in the other thread regarding tolerance ).

I've found that reduction of dose with gabapentin , down to 1200-1500 mg daily in split doses, and taken only 4-5 days outta 7 works best.

Higher doses for long periods of months only managed to bring on adverse reactions for me-- More nerve pain, poor mood, weight gain etc.

By reducing dose and spacing out days of use, Gabapentin has become useful therapeutically once again.

I don't use it recreationally.

 

[darkielass]

love gpt,no anxiety magical,but I'm amazed at the amounts maybe I'm just a baby lol,can you take co codamol or tramadol with gpt,may seem silly question but I'm just a beginner in awe of everyone on here

 

[JacksinPA]

This is my 4th experience with using gabapentin recreationaly. I took 1,000 mg at 6:30 after dinner & another 1,000 mg at 7:00. Three & a half hours later I feel really stoned. It's hard to describe the experience but I find it very pleasant. It is a lot like the effect of smoking weed. But I feel energized & working on the computer is fun.

The high lasted for over 4 hours.

As I learned a few weeks ago, tolerance builds up pretty fast, so this is an experience I plan to have on an occasional basis.

As a side note, I slept very well that night & felt great when I woke in the morning. It is now mid-evening & I feel no withdrawal symptoms.

 

[George27]

Even after 3 days of use, the effect is diminished to near geometric proportions.
I feel that the future will entail Gabapentinoid drugs that do not have this same propensity for inducing withdrawal.

Or an opioid without tolerance and addiction?
A drug is just a tool that works on receptors, and for some receptors there is no workaround.

..... a gapentinoid without the fast tolerance would be a really nice and abusable drug, for me much better than alcohol.
I would try this:
https://en.wikipedia.org/wiki/Mirogabalin

 

[Coolwhip]

Speaking of which, I would really like to get my hands on one of the benzenoid opioids in the tunnel.

 

[D.pharm]

I am on 1200mg of pregabalin a day and the last time I was in the hospital, the ER nurses were skeptical that anyone was prescribed a dose that high. It is fascinating to read about how much more other people posting in this thread are prescribed. My 120 (4 X 300mg capsule monthly allowance is also often questioned when I go to a new pharmacy .
I am aware that an increase in dose is not linear as it relates to bio availability

The FDA, whose opinion on anything doesn't carry much weight with me outlines a maximum dose of 600/mg a day and while obviously physicians are not bound by that it helps me understand the experiences I had with ER nurses and pharmacists when I claimed I was taking a measly 1200mg/day.

Clearly, I am a lightweight.

I have been taking pregabalin for 7 years and it is the only drug I found (and I was previously put on a million other meds before finding gabapentin and then pregabalin). That offered relief from some of the symptoms specific to my menu of mental illnesses.
PTSD
GAD
ADHD
Tx Resistant Depression
Rapid Eye Movement Sleep Behavior Disorder
Reactive Attachment Disorder
Ad infinitum

I am supposed to take all 1200mg before bed and it has been incredibly (miraculously helpful for me personally for anyone who knows what not being able to sleep for 45 years is like) helpful at "simply stopping" my nighttime PTSD flashbacks that had made it impossible to get more than 3-3.5 hours rest any time day or night for over 45 years.
I haven't seen anyone else being prescribed pregabalin for PTSD but I haven't done a comprehensive search of the site either

Trazadone, seroquel, benzos, Z-DRUGS , ssris ,maois, trycyclics,typical/atyical antipsychotics and even phenobarbital had never provided me with any relief for this particular symptom -AT ALL. Well. ketamine would eventually knock me out but I never wanted to go too far down that road.
Gabapentin at twice the dose of my current pregabalin script offered surprisingly little symptomatic relief for me while pregabalin was an instant blessed panacea. ( I personally don't believe those who espouse pregabalin was only manufactured to offer the same benefits of gabapentin at twice the potency and many times the price even though I generally have little regard for or trust in BIG Pharma as a rule.

I was a little woozy each time I titrated up if took the capsules too late and had to deal with a crying baby 2 hours later and felt its recreationally desirable benefits disappeared after a week or so.
But I was blissfully asleep each night on my dose so never thought of it as a recreationally desirable drug.
And frankly a full nights rest free night terrors was more desirable than any high after 45 years.

In the past 7 years, there has been zero tolerance increase with respect to relief my specific symptoms so my dose has remained 1200mg to this day.

I remember being told to titrate up slowly to 1200 mg when first prescribed it in 300mg increments over the first four weeks- (I had been off gabapentin for over a year.)

But me, being me, found out about its recreational benefits a year or so later. Fortunately 900mg offered me similar symptomatic benefits of 1200 mg so I would save up and have a little binge at the end of each month.

I guess because, I was taking three weeks off before playing around with my monthly 25 or 30 extra 300 mg capsules I never felt the desire to push the 4 gram mark.

I would basically just take one every couple of hours until they ran out and fully support the opinions that staggering the doses is the way to go.
I never have experienced any pregabalin withdrawal from either a few days at the 4g mark or when I forgot to pack my meds and abruptly stopped a nightly 9-1200mg daily dose taken every single night that I had been taking for over 6 years. I felt fine on my month long trip with the exception that my night terrors returned by night 4.

How long and how much pregabalin are people taking before they experience withdrawals.?????
Which I understand suck.

I also have ADHD and I noticed a much smoother come up from my morning stimulant medication when pregabalin was taken the night before BUT there was a really, really nice synergy when higher doses of pregabalin where staggered throughout the day. Lisdexamfetamine is already so much smoother than mixed salt amphetamines or methylphenidate but boosted with pregabalin throughout the day it provided significantly increased euphoria, focus, absolutely no edge , with no negative come up or down from the Vyvanse.

YMMV, but can someone offer some phamacodynamic insight as to why this might be?

This is not related to potentiation but someone had asked and another post responded earlier in this thread whether pregabalin might help mitigate some of the horrors of opiate withdrawal.

Again, this is anecdotal and YMMV, but I jumped off buprenorphine at 2mg after a five year run and experienced zero withdrawal symptoms and I never felt anything approaching PAWS.
I am a total crybaby when it comes to withdrawal in general and I know hard core opiate enthusiasts that were forced to taper down to .25mg every other day over a year to have any hope of enduring the apparently relentless and eternal buprenorphine withdrawal process.

My company suddenly transferred me to their office in the Dominican Republic where buprenorphine is illegal and I was scared out of my mind.
Didn't miss a night of sleep, no RLS, fatigue, sweating, mood, anxiety or GI distress. But I think I have enough on my plate as it is LOL
I would put pregabalin in anyone's (loperamide, clonidine, dxm etc) bug out bag of opiate withdrawal essentials.

I am hoping someone can share a link to a study showing the insufflation bio-availability of pregabalin is as poor as is often mentioned in this thread.

My friend swears by this ROA.

Sorry, this meandered so much but thanks if you are still reading.

 

[Runningfox]

I am on 1200mg of pregabalin a day and the last time I was in the hospital, the ER nurses were skeptical that anyone was prescribed a dose that high. It is fascinating to read about how much more other people posting in this thread are prescribed. My 120 (4 X 300mg capsule monthly allowance is also often questioned when I go to a new pharmacy .
I am aware that an increase in dose is not linear as it relates to bio availability

The FDA, whose opinion on anything doesn't carry much weight with me outlines a maximum dose of 600/mg a day and while obviously physicians are not bound by that it helps me understand the experiences I had with ER nurses and pharmacists when I claimed I was taking a measly 1200mg/day.

Clearly, I am a lightweight.

I have been taking pregabalin for 7 years and it is the only drug I found (and I was previously put on a million other meds before finding gabapentin and then pregabalin). That offered relief from some of the symptoms specific to my menu of mental illnesses.
PTSD
GAD
ADHD
Tx Resistant Depression
Rapid Eye Movement Sleep Behavior Disorder
Reactive Attachment Disorder
Ad infinitum

I am supposed to take all 1200mg before bed and it has been incredibly (miraculously helpful for me personally for anyone who knows what not being able to sleep for 45 years is like) helpful at "simply stopping" my nighttime PTSD flashbacks that had made it impossible to get more than 3-3.5 hours rest any time day or night for over 45 years.
I haven't seen anyone else being prescribed pregabalin for PTSD but I haven't done a comprehensive search of the site either

Trazadone, seroquel, benzos, Z-DRUGS , ssris ,maois, trycyclics,typical/atyical antipsychotics and even phenobarbital had never provided me with any relief for this particular symptom -AT ALL. Well. ketamine would eventually knock me out but I never wanted to go too far down that road.
Gabapentin at twice the dose of my current pregabalin script offered surprisingly little symptomatic relief for me while pregabalin was an instant blessed panacea. ( I personally don't believe those who espouse pregabalin was only manufactured to offer the same benefits of gabapentin at twice the potency and many times the price even though I generally have little regard for or trust in BIG Pharma as a rule.

I was a little woozy each time I titrated up if took the capsules too late and had to deal with a crying baby 2 hours later and felt its recreationally desirable benefits disappeared after a week or so.
But I was blissfully asleep each night on my dose so never thought of it as a recreationally desirable drug.
And frankly a full nights rest free night terrors was more desirable than any high after 45 years.

In the past 7 years, there has been zero tolerance increase with respect to relief my specific symptoms so my dose has remained 1200mg to this day.

I remember being told to titrate up slowly to 1200 mg when first prescribed it in 300mg increments over the first four weeks- (I had been off gabapentin for over a year.)

But me, being me, found out about its recreational benefits a year or so later. Fortunately 900mg offered me similar symptomatic benefits of 1200 mg so I would save up and have a little binge at the end of each month.

I guess because, I was taking three weeks off before playing around with my monthly 25 or 30 extra 300 mg capsules I never felt the desire to push the 4 gram mark.

I would basically just take one every couple of hours until they ran out and fully support the opinions that staggering the doses is the way to go.
I never have experienced any pregabalin withdrawal from either a few days at the 4g mark or when I forgot to pack my meds and abruptly stopped a nightly 9-1200mg daily dose taken every single night that I had been taking for over 6 years. I felt fine on my month long trip with the exception that my night terrors returned by night 4.

How long and how much pregabalin are people taking before they experience withdrawals.?????
Which I understand suck.

I also have ADHD and I noticed a much smoother come up from my morning stimulant medication when pregabalin was taken the night before BUT there was a really, really nice synergy when higher doses of pregabalin where staggered throughout the day. Lisdexamfetamine is already so much smoother than mixed salt amphetamines or methylphenidate but boosted with pregabalin throughout the day it provided significantly increased euphoria, focus, absolutely no edge , with no negative come up or down from the Vyvanse.

YMMV, but can someone offer some phamacodynamic insight as to why this might be?

This is not related to potentiation but someone had asked and another post responded earlier in this thread whether pregabalin might help mitigate some of the horrors of opiate withdrawal.

Again, this is anecdotal and YMMV, but I jumped off buprenorphine at 2mg after a five year run and experienced zero withdrawal symptoms and I never felt anything approaching PAWS.
I am a total crybaby when it comes to withdrawal in general and I know hard core opiate enthusiasts that were forced to taper down to .25mg every other day over a year to have any hope of enduring the apparently relentless and eternal buprenorphine withdrawal process.

My company suddenly transferred me to their office in the Dominican Republic where buprenorphine is illegal and I was scared out of my mind.
Didn't miss a night of sleep, no RLS, fatigue, sweating, mood, anxiety or GI distress. But I think I have enough on my plate as it is LOL
I would put pregabalin in anyone's (loperamide, clonidine, dxm etc) bug out bag of opiate withdrawal essentials.

I am hoping someone can share a link to a study showing the insufflation bio-availability of pregabalin is as poor as is often mentioned in this thread.

My friend swears by this ROA.

Sorry, this meandered so much but thanks if you are still reading.

I've researched as much as I could on both lyrica and gabapentin and it APPEARS insufflation is useless as the medication is Taken Up like an amino acid by certain transporters in the gut. (Intestines). Then carried into the brain via this route.
This also explains why staggering doses may help if the patient is taking more than a few hundred mgs a day. The transporters can only carry so much substance at a time and that's where you find those (various amounts) comments saying "anything higher than That is a waste ".

Snorting must be its own addiction/ behavior which provides some kind of benefit to your friend. Call it placebo but if a person truly feels a high from a behavior then it's not "placebo" to him; however I highly doubt any effect of these particular meds is felt via insufflation.